BGP-15
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Ki =57 μM
BGP-15是一种PARP抑制剂。
作为聚ADP核糖聚合酶(PARP)的一组药理学抑制剂,PARP抑制剂被认为是中风和心肌梗塞的一种潜在治疗策略。
体外:之前的研究表明,200 μM的BGP-15可以防止imatinib诱导的氧化损伤,减少高能磷酸盐的消耗,通过阻止p38 MAP激酶和JNK活化来改变imatinib的信号传导效应,还诱导Akt和GSK-3β磷酸化[1]。
体内:体内研究表明,BGP-15改善心脏功能并减少HF和AF两种小鼠模型中的心律失常发作。在这些模型中,BGP-15与IGF1R的磷酸化增加相关。此外,小鼠的心脏特异性IGF1R转基因过表达概括了BGP-15引起的保护。提出者进一步证实,BGP-15对IGF1R的作用可以提供独立于磷酸肌醇3-激酶-Akt和热休克蛋白70的保护[2]。
临床试验:已经安排了BGP-15在2型糖尿病患者中安全性和有效性的临床试验,然而,由于资金支持撤回,本研究现已终止。 (https://clinicaltrials.gov/ct2/show/NCT01069965 term = BGP-15&rank = 1)
参考文献:
[1] Sarszegi Z,Bognar E,Gaszner B,Kónyi A,Gallyas F Jr,Sumegi B,Berente Z. BGP-15, a PARP-inhibitor, prevents imatinib-induced cardiotoxicity by activating Akt and suppressing JNK and p38 MAP kinases. Mol Cell Biochem.2012 Jun;365(1-2):129-37.
[2] Sapra G,Tham YK,Cemerlang N,et al. The small-molecule BGP-15 protects against heart failure and atrial fibrillation in mice. Nat Commun.2014 Dec 9;5:5705.
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 351.27 |
Cas No. | 66611-37-8 |
Formula | C14H24Cl2N4O2 |
Solubility | Soluble in DMSO |
Chemical Name | N-(2-hydroxy-3-(piperidin-1-yl)propoxy)nicotinimidamide dihydrochloride |
SDF | Download SDF |
Canonical SMILES | N=C(NOCC(O)CN1CCCCC1)C2=CN=CC=C2.Cl.Cl |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |